Xelevia mankhwala: malangizo ntchito > Chithandizo ndi kupewa

Amapezeka m'mapiritsi okhala ndi filimu. Mapiritsi okhala ndi kirimu, omwe ali pachithunzithunzi cha filimu mbali ina amalembedwa "277", mbali inayo amakhala osalala.

Chofunikira chachikulu ndi sitagliptin phosphate monohydrate mu Mlingo wa 128,5 mg. Zowonjezera: cellcrystalline cellulose, calcium hydrogen phosphate, croscarmellose sodium, magnesium stearate, magnesium stearyl fumarate. Kuphatikizako kwa kanema kumakhala ndi mowa wa polyvinyl, titanium dioxide, polyethylene glycol, talc, chikasu ndi red iron oxide.

Mankhwalawa amapezeka m'matuza a mapiritsi 14. Phukusi la makatoni mumakhala matuza 2 ndi malangizo ogwiritsira ntchito.

Kumene ndi momwe mungapangire insulin mu matenda a shuga - werengani m'nkhaniyi.

Zotsatira za pharmacological

Adalinganiza zochizira matenda amtundu wachiwiri. Makina ochitapo kanthu amatengera zovuta za enzyme DPP-4. The yogwira thunthu zimasiyana zochita ndi insulin ndi zina antiglycemic wothandizira. Kukumana kwa glucose wodalira insulinotropic timakulitsa.

Pali kuponderezedwa kwa katulutsidwe wa glucagon ndi maselo a pancreatic. Izi zimathandizira kuchepetsa kapangidwe ka shuga m'chiwindi, chifukwa cha zomwe zizindikiro za hypoglycemia zimachepetsedwa. Kuchita kwa sitagliptin cholinga chake ndikulepheretsa hydrolysis ya pancreatic Enzymes. Glucagon secretion imachepetsedwa, potero imalimbikitsa kutulutsa kwa insulin. Poterepa, index ya glycosylated insulin ndi kuchuluka kwa shuga m'magazi kumachepetsedwa.

Xelevia cholinga chake ndikuchiza matenda amtundu wa 2 shuga.

Pharmacokinetics

Mutatha kumwa mapiritsiwo mkati, chinthucho chimayamba kugwira ntchito mwachangu. Kudya kumakhudza mayamwidwe. Kuchuluka kwake kwa magazi kumatsimikizika patatha maola angapo. Bioavailability ndiwambiri, koma kuthekera kumangiriza ku zomanga mapuloteni ndizochepa. Metabolism imachitika m'chiwindi. Mankhwalawa amachotsedwa m'thupi limodzi ndi mkodzo pochita kusefa kwa impso osasinthika komanso mawonekedwe a metabolites ofunikira.

Zizindikiro zogwiritsidwa ntchito

Pali zisonyezo zingapo zachindunji zogwiritsira ntchito mankhwalawa:

monotherapy kusintha kagayidwe ka glycemic kwa odwala omwe ali ndi matenda a shuga a 2,
kuyamba mankhwala ovuta a metformin mtundu 2 matenda ashuga,
mankhwalawa matenda a shuga 2, pamene zakudya ndi zolimbitsa thupi sizigwira ntchito,
zowonjezera insulin
kukonza glycemic control kuphatikiza ndi sulfonylurea zotumphukira,
kuphatikiza mankhwala a shuga a mtundu wachiwiri ndi thiazolidatediones.

Contraindication

Contraindication mwachindunji pakugwiritsa ntchito mankhwalawa, omwe akuwonetsedwa mu malangizo ogwiritsira ntchito, ndi:

Hypersensitivity pamagawo a mankhwala,
mimba ndi mkaka wa m`mawere
wazaka 18
matenda ashuga ketoacidosis,
mtundu 1 shuga
matenda a impso.

Xelevia amagwiritsidwa ntchito pochiza matenda amtundu wa 2 shuga, pomwe zakudya komanso masewera olimbitsa thupi sizikugwira ntchito.

Ndi chisamaliro chachikulu, Xelevia imalembedwa kwa anthu omwe ali ndi vuto lozama komanso lozama laimpso, odwala omwe ali ndi mbiri ya kapamba.

Kutenga Xelevia?

Mlingo ndi nthawi yayitali ya chithandizo zimatengera kuopsa kwa vutolo.

Popanga monotherapy, mankhwalawa amatengedwa koyamba tsiku lililonse la 100 mg patsiku. Mlingo womwewo umawonedwa mukamagwiritsa ntchito mankhwalawa limodzi ndi metformin, insulin ndi sulfonylureas. Mukamapangira zovuta mankhwala, ndikofunikira kuti muchepetse mlingo wa insulin yomwe imatengedwa kuti mupewe kukula kwa hypoglycemia.

Osamwa kawiri mlingo wa mankhwalawa tsiku limodzi. Ndi kusintha kwakukuru paumoyo, kusintha kwa mankhwala kungafunikire. Nthawi zina, mapiritsi theka kapena kotala ndi omwe amapatsidwa, omwe amangokhala ndi zotsatira za placebo. Mlingo wa tsiku ndi tsiku umatha kusiyanasiyana ndikuwonetsa kuwonekera kwa matendawa ndikuyenda bwino kwa mankhwalawa.

Zotsatira zoyipa za Xelevia

Mukamamwa Xelevia, zotsatirazi zimakhala zotsatirazi:

thupi lawo siligwirizana
kusowa kwa chakudya
kudzimbidwa
kukokana
tachycardia
kusowa tulo
paresthesia
kusakhazikika mtima.

Nthawi zina, kuchuluka kwa zotupa m'mimba kumatheka. Mankhwalawa ndi chizindikiro. Woopsa, limodzi ndi kupweteka, hemodialysis amachitidwa.

Gwiritsani ntchito mu ukalamba

Kwenikweni, okalamba odwala safuna kusintha kwa mlingo. Koma ngati matendawo akuipiraipira kapena mankhwalawo samapereka zotsatira zomwe zikuyembekezeka, ndibwino kusiya kumwa mapiritsiwo kapena kusintha mankhwalawo kuti achepe.

Odwala okalamba safuna kusintha kwa mlingo wa Xelevia.

Gwiritsani ntchito pa nthawi yoyembekezera

Palibe chidziwitso chokwanira chokhudza mphamvu ya fetus ya mwana wosabadwayo. Chifukwa chake, kugwiritsa ntchito mankhwalawa pa gestation ndizoletsedwa.

Popeza palibe zambiri zodalirika zokhudzana ndi mankhwalawa ngati mkaka umadutsa mkaka wa m'mawere, ndi bwino kusiya kuyamwitsa ngati chithandizo chimenecho chikufunika.

The ntchito aimpso kuwonongeka

Mankhwala omwe mumalandira adzadalira mtundu wa creatinine chilolezo. Mokulira, amachepetsa mlingo wololedwa. Ngati vuto losakwanira la impso, mlingo woyambirira ungasinthidwe kukhala 50 mg patsiku. Ngati chithandizo sichimapereka chithandizo chofunikira, muyenera kuthetsera mankhwalawo.

Kugwiritsa ntchito kwa vuto la chiwindi

Ndi kufooka pang'ono kwa impso, kusintha kwa mankhwalawa sikofunikira. Mlingo wa tsiku lililonse pamenepa ayenera kukhala 100 mg. Pokhapokha ngati chiwindi chikulephera kwenikweni, mankhwalawa amachitika ndi mankhwalawa.

Ndi chilema chachikulu cha chiwindi, Xelevia sichikuperekedwa.

Mankhwala osokoneza bongo a Xelevia

Palibe milandu ya bongo. Mkhalidwe woopsa wa mankhwala poyizoni ungachitike pokhapokha kumwa limodzi mopitilira 800 mg. Pankhaniyi, zizindikiro za zoyipa zimachulukirachulukira.

Chithandizo chimaphatikizapo kuchiritsa kwam'mimba, kupatsanso mankhwala ena komanso kukonza. Ndikotheka kuchotsa poizoni m'thupi pogwiritsa ntchito dialysis yayitali, chifukwa muyezo hemodialysis imagwira ntchito wofatsa milandu bongo.

Kuchita ndi mankhwala ena

Mankhwalawa amatha kuphatikizidwa ndi metformin, warfarin, njira zina zakutsitsira pakamwa. Ma pharmacokinetics a yogwira ntchito sasintha pogwiritsa ntchito mankhwala ophatikizira a ACE, othandizira ma antiplatelet, mankhwala otsitsa a lipid, beta-blockers ndi calcium blockers.

Izi zimaphatikizaponso mankhwala osokoneza bongo a anti-yotupa, antidepressants, antihistamines, proton pump inhibitors ndi mankhwala ena kuti athetse kusokonekera kwa erectile.

Akaphatikizidwa ndi Digoxin ndi cyclosporine, kuwonjezeka pang'ono kwa kugwiritsidwa ntchito kwa plasma yamagazi kumawonedwa.

Kuyenderana ndi mowa

Simungathe kumwa mankhwalawa ndi mowa. Zotsatira zamankhwala zimachepetsedwa, ndipo zizindikiro za dyspeptic zimangokulira.

Mankhwalawa ali ndi ma analogi angapo ofanana ndi iwo malinga ndi zomwe zimagwiritsidwa ntchito ndi zomwe zimakhala nazo. Zodziwika kwambiri pakati pawo ndi:

Sitagliptin,
Sitagliptin phosphate monohydrate,
Januvius
Yasitara.

Wopanga

Kampani yopanga: Berlin-Chemie, Germany.

Sungani Xelevia kutali ndi ana aang'ono.

Mikhail, wazaka 42, Bryansk

Dokotala adalangiza kuti atenge Xelevia ngati chithandizo chachikulu. Pambuyo pa mwezi wogwiritsa ntchito, shuga yofulumira idachulukirachulukira, isanakwanitse zaka 5, tsopano ifika pa 6-6.5. Zomwe thupi limachita pakulimbitsa thupi zasinthanso. M'mbuyomu, mutayenda kapena kusewera masewera, shuga adagwa kwambiri, ndipo kwambiri, chizindikirocho chinali pafupifupi 3. Mukamamwa Xelevia, shuga pambuyo pakuchita masewera olimbitsa thupi amatsika pang'onopang'ono, kenako amabwerera mwakale. Adayamba kumva bwino. Chifukwa chake ndimalimbikitsa mankhwalawa.

Alina, wazaka 38, Smolensk

Ndimavomereza Xelevia monga chowonjezera cha insulin. Ndakhala ndikudwala matenda a shuga kwa zaka zingapo ndipo ndayesera mankhwala ambiri osakanikirana. Ndimakonda kwambiri izi. Mankhwalawa amangoyankha shuga wambiri. Ngati yatsitsidwa, ndiye kuti mankhwalawo sangathe "kuigwira" ndikuukweza kwambiri. Amachita pang'onopang'ono. Palibe spikes mu shuga masana. Palinso chinthu china chabwino, chomwe sichinafotokozedwe mu malangizo ogwiritsira ntchito: kusintha zakudya. Kulakalaka kumachepetsedwa pafupifupi theka. Izi ndi zabwino.

Mark, wazaka 54, Irkutsk

Mankhwalawo adabwera nthawi yomweyo. Izi zisanachitike, adatenga Januvia. Pambuyo pa iye, sizinali bwino. Patatha miyezi ingapo mutamwa Xelevia, sikuti shuga wokha amabwerera mwakale, komanso thanzi lathunthu. Ndimamva mphamvu zambiri, osafunikira kumangodandaula. Ndinatsala pang'ono kuyiwala kuti hypoglycemia ndi chiani. Shuga samalumpha, kumira ndikukula pang'onopang'ono, pang'ono ndi pang'ono, komwe thupi limayankha bwino.

Kutulutsa mawonekedwe ndi kapangidwe kake

Mlingo wa Xelevia ndi mapiritsi okhala ndi mafilimu: beige, biconvex, ozungulira, osalala mbali imodzi, olembedwa "277" (mu katoni 2 matuza okhala ndi mapiritsi 14) ndi malangizo ogwiritsira ntchito Xelevia.

Piritsi 1:

yogwira thunthu: sitagliptin phosphate monohydrate - 128,5 mg (lofanana ndi zamapuliginin - 100 mg),
othandizira zigawo zikuluzikulu: sodium stearyl fumarate - 12 mg, magnesium stearate - 4 mg, croscarmellose sodium - 8 mg, unbleached calcium hydrogen phosphate - 123.8 mg, microcrystalline cellulose - 123.8 mg,
zokutira filimu: Opadry II beige 85F17438 iron oxide ofiira (E 172) - 0.37%, iron oxide chikasu (E 172) - 3.07%, talc - 14.8%, polyethylene glycol (macrogol 3350) - 20.2% titanium dioxide (E 171) - 21.56%, mowa wa polyvinyl - 40% - 16 mg.

Mankhwala

Xelevia ndi choletsa kusankha kwambiri cha enzyme DPP-4, yomwe imagwira pakamwa komanso chifukwa cha matenda a matenda a shuga 2.

Mphamvu yogwira ya Xelevia (sitagliptin) kuchokera ku analogi ya glucagon-ngati peptide-1 (GLP-1) ndi amylin, cy-glucosidase inhibitors, γ-receptor agonists omwe amathandizidwa ndi peroxisome proliferator (PPAR-γ), insulin, sulfonyurea desivatives. ndi pharmacological zochita. Mwa kuletsa DPP-4, sitagliptin imachulukitsa kuchuluka kwa mahomoni awiri a banja la insretin - GLP-1 ndi insulinotropic polypeptide (HIP) ya glucose.

Mahomoni a banja lino amasungidwa m'matumbo kwa maola 24, poyankha kudya, kuchuluka kwawo kumawonjezeka. Ma incretins ndi gawo limodzi lamomwe timakhazikika pakakhazikitsidwa ka glucose homeostasis. Poyerekeza ndi kuchuluka kwa glucose wabwinobwino kapena wapamwamba, mahomoni am'banja la intretin amathandizira kuwonjezeka kwa insulini komanso chinsinsi chake ndi maselo a pancreatic through maselo kudzera posindikiza njira zomwe zimagwirizanitsidwa ndi cyclic adenosine monophosphate (AMP).

Komanso, GLP-1 imathandizira kubisalira kwa glucagon ndi ma pancreatic α-cell. Kuchepa kwa ndende ya glucagon ndikuwonjezeka kwa insulin kumabweretsa kuchepa kwa kupanga kwa shuga ndi chiwindi, zomwe pamapeto pake zimapangitsa kutsika kwa glycemia. Njira iyi yochitira zinthu imasiyana ndi ya chiberekero cha sulfonylurea, chomwe, ngakhale ndi mpweya wochepa wamagazi, chimalimbikitsa kumasulidwa kwa insulin. Izi zimapangitsa kuwoneka kwa sulfone-inachititsa hypoglycemia osati odwala 2 a mellitus a shuga, komanso mwa athanzi.

Pazakudya zambiri zamagalasi m'magazi, zotsatira zomwe zimaphatikizidwa ndi ma insretins pakuchepa kwa katulutsidwe ka glucagon ndikutulutsa kwa insulin sikuwoneka. HIP ndi GLP-1 sizikhudza kutulutsidwa kwa glucagon poyankha hypoglycemia. Ntchito yama insretins pamankhwala olimbitsa thupi imachepa ndi enzyme DPP-4, yomwe imawachulukitsa mofulumira ndikupanga zinthu zosagwira. Sitagliptin imalepheretsa njirayi, chifukwa chomwe kuchuluka kwa plasma kwa mitundu yogwira ya HIP ndi GLP-1 ikukula.

Mwa kukulitsa zomwe zili m'mapaketi, Xelevia imakulitsa kutulutsa shuga komwe kumadalira glucose ndikuthandizira kuchepetsa kubisika kwa glucagon. Odwala a 2 shuga omwe ali ndi hyperglycemia, kusintha kotereku kwa glucagon ndi insulin kumachepetsa kuchuluka kwa hemoglobin HbA _1C ndi kuchepa kwa shuga m'magazi am'magazi, otsimikiza pamimba yopanda kanthu komanso pambuyo poyesa kupanikizika.

Kutenga muyezo umodzi wa Xelevia mu mtundu 2 wa matenda a shuga kumayambitsa zopinga za ntchito ya DPP-4 kwa maola 24, komwe kumathandizira kuchepetsa kuthamanga kwa glucose, komanso pambuyo poti glucose kapena chakudya, kutsitsa kuchuluka kwa glucagon m'madzi a m'magazi, kuonjezera plasma ndende ya insulin ndi C- peptide, ndikuchulukitsa kuchuluka kwa ma protein omwe amayenda mu GLP-1 ndi ISU mu 2 kapena 3 zina.

Kulephera kwina

Kafukufuku wotseguka wa sitagliptin muyezo wa tsiku ndi tsiku wa 50 mg adachitika kuti aphunzire ma pharmacokinetics mosiyanasiyana madongosolo osalephera aimpso. Odzipereka omwe adaphatikizidwa phunziroli adagawika m'magulu otsatirawa:

odwala ndi aimpso kulephera: creatinine chilolezo (CC) 50-80 ml 1 min,
odwala aimpso kulephera kwapakati: CC 30-50 ml pa 1 min,
odwala omwe amalephera kwambiri aimpso: CC 9 point) palibe. Komabe, poganiza kuti chinthucho chimapukutidwa ndi impso, munthu sayenera kuyembekeza kusintha kwakukulu mu pharmacokinetics mu zochitika zotere.

Ukalamba

M'badwo wa wodwalayo alibe kwambiri matendawa pamankhwala a pharmacokinetic. Poyerekeza ndi odwala ang'onoang'ono, kuchuluka kwa sitagliptin okalamba (azaka zapakati pa 65 mpaka 80) kumakhala kwakukulu ndi pafupifupi 19%. Kutengera zaka, kusintha kwa Xelevia sikumachitika.

Xelevia, malangizo ntchito: njira ndi mlingo

Mapiritsi amatengedwa pakamwa, ngakhale zakudya. Mlingo woyenera wa mankhwalawa ndi piritsi limodzi (100 mg) kamodzi patsiku. Xelevia imagwiritsidwa ntchito mu monotherapy, mwina munthawi yomweyo ndi metformin / sulfonylurea derivatives / PPAR-agonists, kapena metformin ndi sulfonylurea zotengera / metformin ndi PPAR-γ agonists / insulin (wopanda kapena ndi metformin).

Mlingo wa mankhwalawa omwe amagwiritsidwa ntchito nthawi imodzi ndi Xelevia amasankhidwa kutengera mtundu waukulu wa mankhwalawa.

Poyerekeza ndi chithandizo cha mankhwala ophatikizidwa ndi Xelevia omwe ali ndi insulin kapena zotumphukira za sulfonylurea, ndikofunikira kuchepetsa miyambo ya insulin komanso zotumphukira za sulfonylurea kuti muchepetse kuthekera kwa insulin kapena chifukwa cha hypoglycemia.

Mukadumpha mapiritsi, ndikofunikira kuti muwatenge iwo mofulumira momwe wodwala amakumbukirira mlingo womwe wakusowa. Tiyenera kudziwa kuti kugwiritsa ntchito mankhwalawa kawiri pa tsiku lomwelo ndikosavomerezeka.

Kuwongolera kwa dosing regimen yolephera kuchepa kwa impso (CC ≥ 50 ml pa mphindi imodzi, pafupifupi yolingana ndi serum creatinine ndende ≤ 1.5 mg pa 1 dL mwa akazi ndi ≤ 1,7 mg pa 1 dL mwa amuna) sikofunikira.

Odwala omwe ali ndi pakati komanso aimpso kulephera, kusintha kwa mankhwala kwa sitagliptin kumafunika.Popeza palibe chiopsezo chakulekana ndi mapiritsi a Xelevia ndipo samamasulidwa pa 25 kapena 50 mg (koma pokhapokha pa 100 mg), sizingatheke kutsimikizira njira yodalirika ya odwala. Pankhani imeneyi, mankhwala omwe ali m'gulu lino la odwala sanakhazikitsidwe.

Kugwiritsa ntchito sitagliptin motsutsana ndi kulephera kwa impso kumafunika kuwunika kwa impso musanayambe chithandizo komanso nthawi yogwiritsira ntchito.

Pofatsa pang'ono komanso pang'ono pakadutsa chiwindi, komanso odwala okalamba, mlingo wa mankhwalawo sasinthidwa. Kugwiritsa ntchito kwa Xelevia poyang'ana kumbuyo kwa kulephera kwambiri kwa chiwindi sikunafufuzidwe.

Kuyambitsa kuphatikiza mankhwala ndi metformin

Kafukufuku wopangidwa ndi placebo wowongoleredwa ndi masabata 24 adachitidwa poyambira kuphatikiza mankhwala a sitagliptin tsiku lililonse la 100 mg ndi metformin tsiku lililonse la 1000 kapena 2000 mg (50 mg ya sitagliptin + 500 kapena 1000 mg ya metformin 2 kawiri pa tsiku. Malinga ndi zomwe zapezeka, zochitika zosagwirizana ndi kumwa mankhwalawa zimawonedwa pafupipafupi (pafupipafupi ≥ 1%) pagululi lomwe limalandira sitagliptin + metformin kuposa ndi metformin monotherapy. Zotsatira zoyipa m'magulu a sitagliptin + metformin ndi metformin mu monotherapy anali (motero):

matenda otsegula m'mimba - 3.5 ndi 3.3%,
kusanza - 1.1 ndi 0,3%,
mutu - 1.3 ndi 1.1%,
dyspepsia - 1.3 ndi 1.1%,
hypoglycemia - 1.1 ndi 0,5%,
glulence - 1.3 ndi 0,5%.

Kugwiritsa ntchito mosiyanasiyana ndi zotumphukira za sulfonylurea kapena zotumphukira za sulfonylurea ndi metformin

Mu sabata la 24, kafukufuku wowongoleredwa ndi placebo wophatikizidwa kwa 100 mg ya sitagliptin patsiku ndi glimepiride kapena glimepiride ndi metformin, pafupipafupi (ndi pafupipafupi wa ≥ 1%) kukula kwa hypoglycemia kumawonetsedwa poyerekeza ndi gulu lomwe limalandira placebo ndi glimepiride kapena glimepiride ndi metformin. Pafupipafupi kukula kwake kunali 9.5 / 0.9%, motsatana.

Mankhwala oyamba ophatikizira ndi PPAR-γ agonists

Mukamachita kafukufuku wama sabata 24 a mankhwala ophatikiza oyamba ndi sitagliptin muyezo wa tsiku lililonse wa 100 mg ndi pioglitazone tsiku lililonse la 30 mg mgulu lomwe limalandira sitagliptin, zotsatira zoyipa zimawonedwa pafupipafupi (pafupipafupi ≥ 1%) kuposa pagululi lomwe limalandira pioglitazone mu monotherapy . Zomwe zimachitika ndizovuta m'magulu a sitagliptin + pioglitazone ndi pioglitazone mu monotherapy anali (motsatana):

Hypoglycemia: 0,4 ndi 0,8%,
kuchepa kwa asymptomatic m'magazi a shuga m'magazi: 1.1 ndi 0%.

Kuphatikiza mankhwala ndi metformin ndi agonists a PPAR-y

Kafukufuku wovomerezeka ndi placebo adachitika pogwiritsa ntchito 100 mg ya sitagliptin patsiku nthawi yomweyo ndi rosiglitazone ndi metformin ndikuchita nawo magulu awiri - odwala omwe amalandira kuphatikiza ndi mankhwalawa, komanso anthu omwe amalandira kuphatikiza ndi placebo. Malinga ndi zomwe zapezedwa, zotsatirapo zoyipa zimawonedwa pafupipafupi (pafupipafupi ndi ≥ 1%) pagululi lomwe limalandira sitagliptin kuposa gulu lomwe limalandira placebo.

Pa sabata la 18 lowonera m'maguluwa, zoyipa zake zidadziwika ndi pafupipafupi:

kusanza - 1.2 ndi 0%,
mutu - 2,4 ndi 0%,
hypoglycemia - 1,2 ndi 0%,
nseru - 1,2 ndi 1.1%,
matenda otsegula m'mimba - 1.8 ndi 1.1%.

Pa sabata la 54 la kuwonedwa m'magulu awa, zoyipa zambiri zimawonedwa ndi pafupipafupi:

zotumphukira edema - 1,2 ndi 0%,
mutu - 2,4 ndi 0%,
nseru - 1,2 ndi 1.1%,
fungal matenda a pakhungu - 1,2 ndi 0%,
chifuwa - 1.2 ndi 0%,
hypoglycemia - 2.4 ndi 0%,
chapamwamba kupuma thirakiti matenda - 1.8 ndi 0%,
kusanza - 1,2 ndi 0%.

Kuphatikiza mankhwala ndi insulin

Mu kafukufuku wama-24-placebo omwe amayang'aniridwa ndikugwiritsa ntchito mankhwala osakanikirana a 100 mg ya sitagliptin patsiku ndi mlingo wokhazikika wa insulin (popanda kapena ndi metformin), zotsatira zoyipa zimawonedwa pafupipafupi (pafupipafupi ndi ≥ 1%) pagulu lomwe limalandira sentgliptin limodzi ndi insulin (popanda kapena metformin ) kuposa pagulu la placebo ndi insulin (yopanda kapena ya metformin). Zochitika zotsutsa zinali (motsatana):

mutu - 1,2 / 0%,
chimfine - 1.2 / 0,3%,
hypoglycemia - 9.6 / 5.3%.

Kafukufuku wina wa masabata 24, momwe sitagliptin adagwiritsidwira ntchito ngati chida chowonjezera cha mankhwala a insulin (popanda kapena ndi metformin), sizinawonetse zoyipa zilizonse zomwe zimagwirizana ndi kumwa mankhwalawa.

Pancreatitis

Kuwunikira kofotokozedwaku kwa mayeso a 19 awiri akhungu, osasinthika mwanjira zoyeserera zamagwiritsidwe ntchito a sitagliptin muyezo wa tsiku ndi tsiku wa 100 mg kapena mankhwala othandizira (yogwira kapena placebo) adawonetsa kuti zochitika za pancreatitis zosagwirizana ndi zolakwika zili ndi vuto la 0.1 pazaka zana zothandizira odwala pagulu lililonse.

Kupatuka kwakukulu munjira zofunika kapena ma electrocardiograms, kuphatikizapo nthawi yayitali ya QTc, sikunawonedwe ndi sitagliptin.

Sitagliptin Cardiovascular Safety Test Study (TECOS)

TECOS idaphatikizapo odwala 7332 omwe amalandira 100 mg ya sitagliptin patsiku (kapena 50 mg patsiku ngati maziko akuyerekeza kusefukira kwa glomerular anali ≥ 30 ndi 2), komanso odwala 7339 omwe amalandira placebo pagulu la anthu omwe adapatsidwa mankhwala

Mankhwalawa kapena placebo adawonjezeredwa ku chithandizo chokhazikika malinga ndi zomwe zilipo mayiko pakusankha mulingo wa HbA_1C ndi kuwongolera mtima ndi chiopsezo cha zinthu. Odwala onse a 2004 kuyambira azaka 75 adaphatikizidwa pakuwonera, pomwe 970 idalandira sitagliptin, ndipo 1034 idalandira placebo. Zowopsa zonse zoyipa m'magulu onsewa zinali zofanana. Kawuniwuni wamavuto omwe amadza chifukwa cha matenda a shuga, omwe m'mbuyomu adawunikira, adawonetsa zomwe zimachitika pakati pamagulu mutatenga sitagliptin / placebo, kuphatikizapo kuperewera kwaimpso (1.4 / 1.5%) ndi matenda (18, 4 / 17.7%). Zotsatira zoyipa za odwala omwe ali ndi zaka 75 ndi kupitilira zambiri zinali zofanana ndi zomwe anthu ambiri amakhala nazo.

Chiwopsezo cha zigawo za hypoglycemia yayikulu pakati pa odwala omwe adalandira chithandizo chamankhwala "omwe anali ndi cholinga" ndipo omwe adalandira chithandizo cha sulfonylurea ndi / kapena insulin atamwa sitagliptin / placebo anali 2.7 / 2,5% motsatana. Komanso, mwa odwala omwe poyamba sanatenge sulfonylurea ndi / kapena kukonzekera insulin, pafupipafupi anali 1 / 0,7%, motero. Pa nthawi yofunsidwa, ziwonetsero za milandu yotsimikizika ya kapamba akamamwa mankhwalawa inali 0,3 / 0,2%, ndi neoplasms yoyipa - 3,7 / 4%, motero.

Zolemba pambuyo pa kulembetsa

Kuunikira pambuyo pa kulembetsa kugwiritsa ntchito sitagliptin mu monotherapy ndi / kapena kuphatikiza ndi mankhwala ena a hypoglycemic kwawonetsa zowonjezera. Popeza izi zidapezedwa mwakufuna kwa anthu osawerengeka, ubale ndi zomwe zimachitika pothandizidwa ndi izi sizingakhazikike.

Izi zikuphatikiza:

angioedema,
Hypersensitivity zimachitika, kuphatikizapo anaphylaxis,
pruritus / totupa, urticaria, pemphigoid, khungu la vasculitis, zotupa za khungu, kuphatikizapo matenda a Stevens-Johnson,
kapamba pachimake, kuphatikiza mafupa a hemorrhagic ndi necrotic okhala ndi / popanda kupha,
kuwonongeka kwaimpso, kuphatikiza pachimake kukanika kwa impso (nthawi zina, kuyimba kwa mankhwalawa kumafunikira),
chapamwamba kupuma thirakiti matenda
nasopharyngitis,
kusanza, kudzimbidwa,
mutu
arthralgia, myalgia,
kupweteka miyendo, kumbuyo.

Zosintha zasayansi

M'maphunziro ambiri azachipatala, panali kuwonjezeka pang'ono kwa chiwerengero cha leukocyte mwa odwala omwe amalandila sitagliptin (100 mg patsiku) poyerekeza ndi gulu la placebo (200 μl pa avareji, kumayambiriro kwa mankhwala chizindikiro chinali 6600 μl), zomwe ndi chifukwa cha kuchuluka kwa neutrophils.

Kuwonjezeka pang'ono kwa uric acid okhutira (ndi 0,2 mg pa 1 dl) adapezeka ndi 100 ndi 200 mg ya sitagliptin patsiku poyerekeza ndi placebo. Asanayambe chithandizo, pafupifupi mtengo anali 5-5,5 mg pa 1 dL. Palibe milandu ya gout yomwe yanenedwapo.

Kunali kuchepa pang'ono pang'onopang'ono mu phosphatase yonse yamchere pagulu lomwe limalandira mankhwalawo, poyerekeza ndi gulu la placebo (pafupifupi 5 IU pa 1 lita, pafupifupi, isanayambike mankhwala, ndende inali 56 mpaka 62 IU pa lita imodzi), yomwe idalumikizidwa ndi yaying'ono Kuchepa kwa mafupa a enzyme.

Zosintha mu magawo a ma laboratori sizimawonedwa ngati zazama.

Hypoglycemia

Malinga ndikuwunika kwachipatala, kuchuluka kwa hypoglycemia panthawi ya monotherapy ndi sitagliptin kapena chithandizo chake munthawi yomweyo ndimankhwala osayambitsa matenda amtunduwu (pioglitazone, metformin) anali ofanana ndi omwe anali mgululi la placebo. Monga ndimankhwala ena a hypoglycemic, hypoglycemia imachitika mu nthawi ya makonzedwe a Xelevia osakanikirana ndi mankhwala a sulfonylurea kapena insulin. Kuchepetsa mwayi wa sulfon-in ikiwayambitsa hypoglycemia, mlingo wa zotuluka za sulfonylurea umachepetsedwa.

Chithandizo cha odwala okalamba

Chitetezo ndikuwoneka bwino kwa Xelevia pamavuto azachipatala odwala okalamba (odwala 409) azaka zopitilira 65 anali ofanana ndi omwe ali mgulu la odzipereka osakwana zaka 65. Pankhaniyi, kusintha mtundu wa mankhwalawa kutengera zaka zomwe wodwala safunika. Tiyenera kukumbukira kuti odwala okalamba amakonda kukhala ndi impso. Chifukwa chake, pamaso pa kulephera kwambiri kwa impso m'gulu lino, monga mwa ena onse, mlingo wa sitagliptin umasinthidwa.

Mu kafukufuku wa TECOS, odzipereka amalandira sitagliptin pa mlingo wa tsiku ndi tsiku wa 100 mg (kapena 50 mg patsiku ndi mtengo woyambirira wa pafupifupi glomerular filtration rate ≥ 30 ndi 2) kapena placebo. Adawonjezeredwa kuchizolowezi chogwirizana molingana ndi miyezo yapadziko lonse yotsimikiza milingo ya HbA._1C ndi kuwongolera mtima ndi chiopsezo cha zinthu. Pamapeto pa nthawi yophunzira (zaka zitatu) mwa odwala matenda ashuga a 2, kumwa mankhwalawa kuwonjezera pa mankhwalawa sikukukulitsa chiyembekezo chachipatala chifukwa cha kulephera kwa mtima (chiopsezo cha 1, 95% chidaliro - kuyambira 0.83 mpaka 1.2, p = 0.98 chifukwa chosiyana pamafupipafupi pamavuto) kapena chiwopsezo cha zotsatira zoyipa kuchokera munthawi yamtima (chiwopsezo cha chiopsezo - 0.98, 95% chidule pakadalira - kuyambira 0.89 mpaka 1.08, p CYP) 2C8, CYP 2C9 ndi CYP 3 A 4. Malinga ndi data ya vitro , sichimalepheretsa CYP 1A2, CYP 2B6, CYP 2C19 ndi CYP 2 D 6 isoenzymes ndipo siziwalimbikitsa CYP 3 A 4 isoenzyme.

Kugwiritsa ntchito metformin kosakanikirana ndi sitagliptin, kusintha kwakukulu pama parachetinetic kwachiwiri sikunawonedwe mwa odwala omwe ali ndi matenda a shuga 2.

Zomwe zimapezeka pa kuchuluka kwa anthu omwe ali ndi vuto la shuga 2 zimawonetsa kuti chithandizo chofanana sichikukhudza kwambiri pharmacokinetics ya mankhwalawa. Kafukufukuyu adawerengera mankhwala omwe nthawi zambiri amalembera mtundu wachiwiri wa matenda ashuga, kuphatikizapo:

β-blockers
lipid-kuchepetsa mankhwala (monga ezetimibe, fibrate, statins),
antidepressants (monga sertraline, fluoxetine, bupropion),
antiplatelet agents (mwachitsanzo, clopidogrel),
antihistamines (mwachitsanzo cetirizine),
mankhwala ochizira erectile dysfunction (mwachitsanzo sildenafil),
mankhwala osapweteka a antiidal (monga celecoxib, diclofenac, naproxen),
proton pump inhibitors (monga lansoprazole, omeprazole),
antihypertensive mankhwala (monga hydrochlorothiazide, slowly calcium blockers, angiotensin II receptor antagonists, angiotensin kutembenuza enzyme inhibitors).

Kukula pang'ono kwa AUC ndi C _m_Ah digoxin (pofika 11 ndi 18%, motero) adadziwika ndi kuphatikiza kwake ndi sitagliptin. Kukula kumeneku sikumawerengedwa kuti ndikofunika m'thupi. Ndi kuphatikiza pamodzi, kusintha kwa mlingo sikulimbikitsidwa.

Kuchulukitsa kwa AUC ndi C _m_Ah Sitagliptin (29 ndi 68%, motero) adawonedwa akamagwiritsa ntchito mlingo wa 100 mg molumikizana ndi kipimo chimodzi cha cyclosporine (choletsa choletsa cha P-glycoprotein) pakukonzekera kwa pakamwa pa mlingo wa 600 mg. Kusintha kwamankhwala mu pharmacokinetic mawonekedwe a mankhwalawa sikuwoneka ngati ofunika kwambiri. Mukamagwiritsa ntchito kuphatikiza ndi cyclosporine kapena P-glycoprotein inhibitor (mwachitsanzo, ketoconazole), sizikulimbikitsidwa kuti musinthe mlingo wa Xelevia.

Malinga ndi kuchuluka kwa anthu omwe amapezeka mu pharmacokinetic kwa odwala komanso odzipereka athanzi (N = 858) kwa mankhwala osiyanasiyana (N = 83, pafupifupi theka lawo lomwe limatulutsidwa kudzera mu impso), zinthuzi sizinawakhudze kwambiri pharmacokinetics ya sitagliptin.

Analogs aku Xelevia ndi Yasitara, Sitagliptin phosphate monohydrate, Januvia.

Zizindikiro ndi contraindication

Chizindikiro chakugwiritsa ntchito "Xelevia" ndi:

kuchepa mphamvu ya munthu wodwala matenda ashuga kwa hypoglycemia motsogozedwa ndi neuropathy kapena mavuto ena azaumoyo,
kudziwa tsogolo la hypoglycemia usiku,
ukalamba
kufunikira kwa chidwi chowongolera poyendetsa kapena kugwiritsa ntchito njira zowerengeka,
pafupipafupi matenda a hypoglycemia pamene akumwabe sulfonylurea.

Musanatenge, ndikofunikira kuti muzidziwitsa zolakwika. Izi zikuphatikiza:

wokhala ndi mwana,
mtundu 1 shuga
matenda ashuga ketoacidosis, osakwana zaka 18,
aimpso kulephera kwa wowongoletsa kapena owopsa mawonekedwe.

Chifukwa cha kuchepa kwa maphunziro olamulidwa zokhudzana ndi kufunikira ndi chitetezo cha mankhwalawa kwa amayi apakati, Xelevia siyikulimbikitsidwa kuti mugwiritse ntchito panthawi yapakati. Komanso kuthekera kwa kutulutsa kwawo pamodzi ndi mkaka wa m'mawere sikunaphunzire, chifukwa chake, ndi mkaka wa m`mawere, ndizophatikizika.

Mlingo ndi bongo

Mlingo woyenera wa mankhwalawa ndi 100 mg 1 nthawi patsiku. Amatengedwa ngati pakamwa ngati mankhwala osakanikirana kapena ali ndi chowonjezera ndi metformin kapena mankhwala okhala ndi zinthu zina zogwira ntchito. Kumwa mankhwalawa sikugwirizana ndi chakudya. Mlingo wa "Xelevia" ndi mankhwala ena, chiwerengero chawo chimakhazikitsidwa ndi adotolo poganizira malingaliro a malangizowo

Ngati mukusowa piritsi, ndikulimbikitsidwa kuti muzimwa mofulumira mukangokumbukira izi. Mu tsiku limodzi amaletsedwa kumwa kawiri mlingo wa mankhwalawa.

M'mayesero azachipatala mwa odzipereka athanzi, mankhwalawa pamlingo waukulu wa 800 mg wa odwala matenda ashuga anali wololera. Zosintha zochepa pazowonetsa sizofunikira. Mlingo pamwambapa 800 mg sunaphunzire. Zotsatira zoyipa mutatenga 400 mg ya "Xelevia" kwa masabata 4 sizinapezeke.

Koma, ngati bongo pazifukwa zilizonse zachitika, wodwalayo samva bwino, ndiye kuti bungwe la zochitika zotere liyenera:

kuchotsa mankhwala osatulutsidwa m'mimba,
kuwunika mayendedwe, kuphatikizapo kuwunika ntchito za mtima kudzera mu ECG,
kuchita kukonza kukonza.

The yogwira mankhwala sitagliptin salemala bwino. Ndi 13.5% yokha yomwe imachotsedwa pakapita maola anayi. Amangoikidwa ngati mwayi womaliza.

Njira yayikulu yothandizira gawo lina la mankhwala kuchokera mthupi ndi kudzera mu impso. Kwa odwala omwe ali ndi matenda a impso, Mlingo umayikidwa pakati, koma vuto la impso limachepa:

kulephera koyenera kapena koopsa
gawo kudwala matenda aimpso.

Pomaliza

Malinga ndi kufotokozera kwa mankhwalawa ndikuwunika za mankhwalawo, titha kunena kuti ndizothandiza komanso zimathandizira odwala. Ubwino wosasinthika ndi kusakhalapo kwathunthu kwa zotsatira zoyipa m'thupi. Mwachilengedwe, munthu sangathe kusankha mankhwalawa, komanso kuphatikiza koyenera ndi mankhwala ena, popanda kuvulaza thanzi lake. Kuti muchite izi, muyenera kulumikizana ndi endocrinologist, osachita mankhwala othandizira.

Kupanga ndi mawonekedwe a kumasulidwa

Piritsi - Piritsi limodzi:

Mphamvu yogwira: sitagliptin phosphate monohydrate - 128,5 mg, yomwe imagwirizana ndi zomwe sitagliptin - 100 mg,
Omwe amathandizira: microcrystalline cellulose - 123.8 mg, osaphatikizika calcium hydrogen phosphate - 123.8 mg, croscarmellose sodium - 8 mg, magnesium stearate - 4 mg, sodium stearyl fumarate - 12 mg,
kapangidwe ka sheath: opadry II beige, 85F17438 - 16 mg (polyvinyl mowa - 40%, titanium dioxide (E171) - 21.56%, macrogol 3350 (polyethylene glycol) - 20.2%, talc - 14.8%, iron iron oxide (E172) - 3.07% , red oxide red (E172) - 0,37%).

14 ma PC. - matuza (2) - mapaketi a makatoni.

Mapiritsi, okhala ndi chipolopolo cha beige, amakhala ozungulira, a biconvex, olembedwa "277" mbali imodzi ndi osalala mbali inayo.

Mankhwala Xelevia (sitagliptin) ndi yogwira pakamwa, ndi choletsa kusankha kwa pulotidyl peptidase-4 (DPP-4), yopanga matenda a shuga 2. Sitagliptin amasiyana mu kapangidwe ka mankhwala ndi zochita za pharmacological kuchokera ku analogi ya glucagon-peptide-1 (GLP-1), insulini, zotumphukira za sulfonylurea, biguanides, gamma receptor agonists yokhazikitsidwa ndi peroxisome proliferator (PPAR-γ), alpha-glucosidase. Mwa kuletsa DPP-4, sitagliptin imachulukitsa kuchuluka kwa mahomoni awiri a banja la ma impretin: GLP-1 ndi insulinotropic polypeptide (HIP) ya glucose. Mahomoni a banja la insretin amatulutsidwa m'matumbo masana, kupendekera kwawo kumawonjezeka chifukwa chodya zakudya. Ma incretins ndi gawo limodzi lamomwe timakhazikika pakakhazikitsidwa ka glucose homeostasis. Pakukhazikika kwachilengedwe kapena kukwera kwa glucose, mahomoni am'banja la intretin amathandizira kuwonjezeka kwa insulin, komanso chinsinsi chake ndi maselo a pancreatic beta chifukwa chakuwonetsa ma intracellular ma processor omwe amayenderana ndi cyclic adenosine monophosphate (AMP).

GLP-1 imathandizanso kupondereza kuchuluka kwa katulutsidwe ka glucagon ndi maselo a pancreatic alpha. Kuchepa kwa ndende ya glucagon poyang'ana kumbuyo kwa kuchuluka kwa insulini kumathandizira kuchepetsa kupanga kwa chiwindi, komwe kumapangitsa kutsika kwa glycemia. Njira iyi yochitira zinthu imasiyana ndimapangidwe a zochita za sulfonylurea, zomwe zimapangitsa kuti magazi atulutse magazi ochepa, omwe amayamba chifukwa cha kukula kwa sulfone-hypoglycemia osati mwa odwala a mtundu 2 shuga, komanso odwala athanzi.

Pokhala ndi shuga wambiri m'magazi, zotsatira zomwe zimaphatikizidwa ndi ma insulin kutulutsidwa kwa insulin ndi kuchepa kwa katulutsidwe ka glucagon sizimawonedwa. GLP-1 ndi HIP sizikhudza kutulutsidwa kwa glucagon poyankha hypoglycemia. Pansi pa zochitika zathupi, ntchito ya ma impretins imachepetsedwa ndi enzyme DPP-4, yomwe hydrolyzes imapangika mwachangu ndikupanga zinthu zosagwira.

Sitagliptin imalepheretsa hydrolysis ya ma impretins ndi enzyme DPP-4, potero kuwonjezera kuchuluka kwa plasma kwa mitundu yogwira ya GLP-1 ndi HIP. Powonjezera kuchuluka kwa ma insretins, sitagliptin imakulitsa kutulutsa shuga komwe kumadalira glucose ndikuthandizira kuchepetsa kubisala kwa glucagon. Odwala omwe ali ndi matenda a shuga a mtundu wachiwiri omwe amakhala ndi hyperglycemia, kusintha kumeneku kwa insulin ndi glucagon kumapangitsa kuchepa kwa ndende ya glycosylated hemoglobin HbA1C komanso kutsika kwa plasma ndende ya glucose, yotsimikizika pamimba yopanda kanthu komanso pambuyo poyesa kupanikizika.

Odwala omwe ali ndi matenda a shuga 2 amisonitus, kutenga mlingo umodzi wa Xelevia kumabweretsa zolepheretsa zochitika za enzyme DPP-4 kwa maola 24, zomwe zimapangitsa kuti chiwopsezo cha kuzungulira kwa ma protein a GLP-1 ndi HIP chichitike ndi 2-3, kuwonjezeka kwa plasma ndende ya insulin ndi C- peptide, kuchepa kwa kuchuluka kwa glucagon m'madzi am'magazi, kuchepa kwa glucose othamanga, komanso kuchepa kwa glycemia pambuyo poyatsira shuga kapena kutsitsa chakudya.

Ma pharmacokinetics a sitagliptin afotokozedwa kwathunthu mwa anthu athanzi komanso odwala matendawa a mtundu wa 2. Mwa athanzi, pambuyo pakamwa makonzedwe a 100 mg a sitagliptin, kuyamwa mwachangu kwa mankhwalawa kumawonedwa ndi kuchuluka kwakukulu (Cmax) kuyambira 1 mpaka maola 4 kuyambira nthawi ya makonzedwe. Dera lomwe limasungidwa nthawi yayitali (AUC) limawonjezeka molingana ndi kuchuluka kwa mankhwalawo ndipo mu maphunziro abwino ndi 8.52 μmol / L * ola pamene atengedwa 100 mg pamlomo, Cmax ndi 950 nmol / L Plasma AUC ya sitagliptin inakula ndi pafupifupi 14% pambuyo pa mlingo wotsatira wa 100 mg ya mankhwalawa kuti apeze gawo lofanana pambuyo atamwa koyamba. Ma intra- komanso intersubject cosefficients a sitagliptin AUC anali osadziwika.

Mtheradi bioavailability wa sitagliptin pafupifupi 87%. Popeza kudya kophatikizana kwa sitagliptin ndi zakudya zamafuta sizimakhudza mankhwala a pharmacokinetics, Xelevia ya mankhwala imatha kutumikiridwa mosasamala za chakudya.

Kuchulukitsa kwapakati pamagawidwe ofanana pambuyo pa gawo limodzi la 100 mg ya sitagliptin mwa odzipereka athanzi ndi pafupifupi 198 l. Gawo la sitagliptin lomwe limamangiriza mapuloteni a plasma ndilotsika kwambiri 38%.

Pafupifupi 79% ya sitagliptin amachotsedwa osasinthika ndi impso. Kachigawo kochepa chabe kamankhwala kamene kamalandiridwa m'thupi kamapukusidwa.

Pambuyo pa 14C yolembedwa kuti sitagliptin mkati, pafupifupi 16% ya ma radiogigiptin a radiowork anamuchotsa monga ma metabolites. Zotsatira za metabolites 6 za sitagliptin zidapezeka, mwina sizingokhala ndi DPP-4 zoletsa. Kafukufuku wa in vitro awulula kuti ma isoenzymes oyambirira omwe akukhudzidwa ndi metabolism ochepa a sitagliptin ndi CYP3A4 ndi CYP2C8.

Pambuyo pa makonzedwe a 14C olembedwa kuti sitagliptin kukhala odzipereka athanzi, pafupifupi 100% ya sitagliptin yomwe idatumizidwa idachotsedwa: 13% kudzera m'matumbo, 87% ndi impso mkati mwa sabata limodzi atatha kumwa mankhwalawo. Kuthetsa theka la moyo wa sitagliptin mwa makonzedwe amkamwa a 100 mg pafupifupi maola 12.4; chilolezo cha impso ndi pafupifupi 330 ml / mphindi.

Kukula kwa sitagliptin kumachitika makamaka chifukwa cha impso pogwiritsa ntchito njira yoteteza tinthu tating'onoting'ono. Sitagliptin ndi gawo logwiritsira ntchito ma transion of organic aanthu amtundu wachitatu (hOAT-3), omwe angatenge nawo gawo la impgionis ya impso. Mwachidziwitso, kuphatikiza kwa hOAT-3 pakuyendetsa sitagliptin sikunaphunzire. Sitagliptin ndi gawo laling'ono la p-glycoprotein, lomwe limathanso kutenga nawo gawo pazakudya za sitagliptin ndi impso. Komabe, cyclosporin, choletsa p-glycoprotein, sichinachepetse chilolezo cha sitagliptin.

Pharmacokinetics m'magulu awiri odwala:

Odwala aimpso kulephera:

Kafukufuku wotseguka wa sitagliptin pa mlingo wa 50 mg patsiku adachitika kuti aphunzire mankhwala ake a pharmacokinetics mwa odwala omwe ali ndi madigiri osiyanasiyana azovuta zamkati. Odwala omwe amaphatikizidwa ndi phunziroli adagawika m'magulu a odwala omwe amalephera kupweteka kwapafupa (kulengedwa kwa creatinine kuchokera 50 mpaka 80 ml / min), chilolezo (cha mtundu wa creatinine kuyambira 30 mpaka 50 ml / min) ndi kulephera kwakukulu kwa aimpso (creatinine chilolezo chosakwana 30 ml / min) , komanso ndi terminal siteji ya aimpso kulephera kwa chiwindi.

Odwala omwe ali ndi vuto lofooka la impso, panalibe kusintha kwakukulu pamatenda a plasma a sitagliptin poyerekeza ndi gulu loyang'anira odzipereka athanzi.

Kuwonjezeka kawiri kwa sitagliptin AUC poyerekeza ndi gulu loyang'anira kunawonedwa mwa odwala omwe amalephera kupezeka bwino aimpso, kuwonjezeka kwaposachedwa kanayi kwa AUC kumawonedwa mwa odwala omwe amalephera kwambiri aimpso, komanso kwa odwala omwe amalephera komanso amalephera. Sitagliptin adachotsedwa pang'ono ndi hemodialysis: 13.5% yokha ya mankhwalawo amachotsedwa m'thupi panthawi ya dialysis ya maola atatu.

Chifukwa chake, kuti tikwaniritse kuchiritsira kwa kuchuluka kwa sitagliptin m'magazi am'magazi (ofanana ndi omwe odwala omwe ali ndi vuto laimpso) odwala omwe ali ndi pakati komanso aimpso kulephera, kusintha kwa mankhwala kumafunika.

Odwala omwe ali ndi vuto la chiwindi:

Odwala omwe ali ndi vuto lochepa la hepatic (7-16 point on the Child-Pugh wadogo), AUC ndi Cmax ya sitagliptin omwe ali ndi mlingo umodzi wowonjezera wa 100 mg pafupifupi 21% ndi 13%, motero. Chifukwa chake, kusinthaku kwa mankhwalawa kuti kufewetse chiwindi pakapita sikofunikira.

Palibe chidziwitso chachipatala pakugwiritsa ntchito sitagliptin kwa odwala omwe ali ndi vuto lolemera la hepatic (oposa 9 mfundo pamiyeso ya Mwana-Pugh). Komabe, chifukwa chakuti sitagliptin adachotsa impso, munthu sayenera kuyembekeza kusintha kwakukulu mu pharmacokinetics ya sitagliptin mwa odwala omwe ali ndi vuto lotupa la hepatic.

Zaka za odwala sizinakhale ndi vuto lililonse pamawonekedwe a pharmacokinetic magawo a sitagliptin. Poyerekeza ndi odwala achichepere, odwala okalamba (azaka 65-80) ali ndi ndende yokhala ndi sitaglin pafupifupi pafupifupi 19%. Palibe kusintha kwa mlingo malinga ndi msinkhu wofunikira.

Oral hypoglycemic mankhwala.

Zotsatira zoyipa za Xelevia

Sitagliptin nthawi zambiri imalekeredwa limodzi mu monotherapy komanso kuphatikiza mankhwala ena a hypoglycemic. M'mayeso azachipatala, zochitika zonse zomwe zimachitika, komanso pafupipafupi kuperewera kwa mankhwala chifukwa cha zovuta, zinali zofanana ndi zomwe zili ndi placebo.

Malinga ndi maphunziro 4 omwe amayendetsedwa ndi placebo - masabata 18-24) a sitagliptin patsiku la 100-200 mg ngati njira imodzi kapena mankhwala ophatikizana ndi metformin kapena pioglitazone, palibe zoyipa zomwe zimakhudzana ndi mankhwala omwe adawerengedwa, zomwe zimakonda kupitilira 1% pagulu la odwala kutenga sitagliptin. Mbiri ya chitetezo chamtundu wa 200 mg tsiku ndi tsiku chinali chofanana ndi mbiri ya chitetezo cha tsiku ndi tsiku cha 100 mg.

Kusanthula kwa deta yomwe idapezedwa pamayeso azachipatala omwe ali pamwambawa adawonetsa kuti ziwonetsero zonse za hypoglycemia mwa odwala omwe amatenga sitagliptin zinali zofanana ndi placebo (sitagliptin 100 mg-1.2%, sitagliptin 200 mg-0.9%, placebo - 0,9%). Pafupipafupi pazochitika zoyipa za m'mimba pakamatenga katemera wa zigawo zisanu ndi ziwiri anali ofanana ndi omwe amapezeka ndi placebo (kupatula pafupipafupi kupezeka kwa mseru mukamamwa Besgliptin pa 200 mg patsiku: kupweteka kwam'mimba (sitagliptin 100 mg - 2) , 3%, sitagliptin 200 mg - 1.3%, placebo - 2.1%, mseru (1.4%, 2.9%, 0.6%), kusanza (0,8%, 0,7% , 0.9%), matenda am'mimba (3.0%, 2.6%, 2.3%).

M'maphunziro onse, mayendedwe osokoneza bongo a hypoglycemia adalembedwa pamaziko a ripoti zonse za matenda a hypoglycemia, kufanana kwa kuchuluka kwa shuga wamagazi sikufunika.

Kuyambitsa kuphatikiza mankhwala ndi metformin:

Mu sabata la 24, kafukufuku wowongolera wa placebo wowongolera poyambira kuphatikiza mankhwalawa ndi sitagliptin tsiku lililonse la 100 mg ndi metformin tsiku lililonse la 1000 mg kapena 2000 mg (sitagliptin 50 mg + metformin 500 mg kapena 1000 mg x 2 pa tsiku) pagulu la mankhwala ophatikiza Poyerekeza ndi gulu la Metformin monotherapy, zochitika zotsatirazi zidawonedwa:

Zotsatira zoyipa zomwe zimachitika pakumwa mankhwalawa zimawonedwa pafupipafupi & gt1% mu gulu la chithandizo cha sitagliptin ndipo nthawi zambiri kuposa gulu la mankhwalawa mu monotherapy: matenda am'mimba (sitagliptin + metformin - 3.5%, metformin - 3.3%), dyspepsia (1, 3%, 1.1%), kupweteka kwam'mutu (1.3%, 1.1%), flatulence (1.3%, 0.5%), hypoglycemia (1.1%, 0.5%), kusanza (1.1%, 0.3%).

Kuphatikiza ndi zotumphukira za sulfonylurea kapena zotumphukira za sulfonylurea ndi metformin:

Pakufufuza kwamankhwala kwakanthawi kwamasamba 24 ka mankhwala osakanikirana ndi sitagliptin (mlingo wa tsiku ndi tsiku wa 100 mg) ndi glimepiride kapena glimepiride ndi metformin, zochitika zotsatirazi zimawonedwa m'gululi la mankhwala omwe amapezeka poyerekeza ndi gulu la odwala omwe akutenga placebo ndi glimepiride kapena glimepiride ndi metformin:

Zotsatira zoyipa zomwe zimachitika pakumwa mankhwala zimawonedwa pafupipafupi & gt1% mu gulu la mankhwalawa ndi sitagliptin ndipo nthawi zambiri kuposa mankhwala omwe amaphatikizidwa ndi placebo: hypoglycemia (sitagliptin - 9.5%, placebo - 0,9%.

Njira zoyambirira zophatikizira ndi PPAR-γ agonists:

Mu kafukufuku wa masabata 24 woyambitsa kuphatikiza mankhwalawa ndi sitagliptin muyezo wa tsiku ndi tsiku wa 100 mg ndi pioglitazone tsiku lililonse la 30 mg, zochitika zotsatirazi zinaonedwa mu gulu la mankhwala osakanikirana poyerekeza pioglitazone monotherapy:

Zotsatira zoyipa zomwe zimachitika pakumwa mankhwala zimawonedwa pafupipafupi & gt1% mu gulu la mankhwala a sitagliptin ndipo nthawi zambiri kuposa gulu la mankhwalawa la pioglitazone mu monotherapy: kuchepa kwa magazi a glucose (seksllinin + pioglitazone - 1.1%, pioglitazone - 0%) Hypoglycemia (0,4%, 0,8%).

Kuphatikiza ndi agonists a PPAR-y ndi metformin:

Malinga ndi kafukufuku yemwe amayang'aniridwa ndi placebo pochiza sitagliptin (mlingo wa tsiku ndi tsiku wa 100 mg) osakanikirana ndi rosiglitazone ndi metformin m'gulu laophunzira mankhwala, zochitika zotsatirazi zimawonedwa poyerekeza ndi gulu la odwala omwe akutenga placebo srosiglitazone ndi metformin:

Pa sabata la 18 la kuwunika:

Zotsatira zoyipa zomwe zimachitika pakumwa mankhwalawa zimawonedwa pafupipafupi & gt1% mu gulu la mankhwalawa ndi sitagliptin ndipo nthawi zambiri kuposa momwe amaphatikizidwira mankhwala a placebo: mutu waching'alang'ala (sitagliptin - 2.4%, placebo - 0.0%), kutsekula m'mimba (1.8 %, 1.1%), nseru (1.2%, 1.1%), hypoglycemia (1.2%, 0,0%), kusanza (1,2%, 0,0%).

Pa milungu 54 yowonera:

Zotsatira zoyipa zomwe zimagwirizana ndi kumwa mankhwalawa zimawonedwa pafupipafupi & gt1% mu gulu la mankhwalawa ndi sitagliptin ndipo nthawi zambiri kuposa mankhwala omwe amaphatikizidwa ndi placebo: kupweteka kwa mutu (sitagliptin - 2.4%, placebo - 0.0%), hypoglycemia (2.4 %, 0,0%), matenda opatsirana am'mapapo apakati (1.8%, 0,0%), nseru (1.2%, 1.1%), chifuwa (1,2%, 0,0%), fungal matenda a pakhungu (1,2%, 0,0%), zotumphukira edema (1.2%, 0,0%), kusanza (1.2%, 0.0%).

Kuphatikiza ndi insulin:

Mu sabata la 24, kafukufuku wowongolera wa placebo wophatikiza mankhwalawa ndi sitagliptin (tsiku lililonse mlingo wa 100 mg) ndi kuchuluka kwa insulin (yokhala ndi metformin kapena yopanda metformin) pagulu la mankhwala omwe amapezeka poyerekeza ndi gulu la odwala omwe akutenga placebo ndi insulin (okhala ndi kapena opandaformform), zochitika zotsatirazi:

Zotsatira zoyipa zomwe zimagwirizana ndi kumwa mankhwalawa zimawonedwa pafupipafupi & gt1% mu gulu la chithandizo cha sitagliptin ndipo nthawi zambiri kuposa gulu la mankhwala a insulin (lomwe lili ndi kapena popanda metformin): hypoglycemia (sitagliptin + insulin (yokhala ndi kapena metformin) - 9.6%, placebo + insulini (wokhala ndi kapena wopanda metformin) - 5.3%), chimfine (1.2%, 0,3%), mutu (1,2%, 0,0%).

Kafukufuku wina wa masabata a 24, pomwe odwala adalandira sitagliptin monga njira yowonjezera yothandizira mankhwala a insulini (omwe ali ndi kapena popanda metformin), palibe zoyipa zomwe zimachitika chifukwa chomwa mankhwalawa pafupipafupi & gt1% pagulu lachipatala la sitagliptin (pa 100 mg ,, nthawi zambiri kuposa gulu la placebo.

Pakuwunika kochulukirapo kwa anthu 19 omwe ali ndi khungu mosavutikira amayesa kugwiritsa ntchito mankhwala a sitagliptin tsiku lililonse la 100 mg kapena mankhwala othandizira (yogwira kapena placebo), zochitika za pancreatitis zosagwirizana ndizochita 100 zilizonse pazaka zana zamankhwala odwala.

Palibe kupatuka kwakuthupi kwamankhwala ofunikira kapena zofunikira za ECG (kuphatikiza nthawi yanthawi ya QTc) zomwe zimawonedwa panthawi ya mankhwala a sitagliptin.

Sitagliptin Cardiovascular Safety Assessment Study (TECOS):

Kafukufukuyu pamatenda a mtima a sitagliptin (TECOS) akuphatikiza odwala 7332 omwe amatenga sitagliptin 100 mg patsiku (kapena 50 mg patsiku ngati maziko akuyerekeza kuchuluka kwa kusefa kwa glomerular (eGFR) anali & gt30 ndi & lt50 ml / mphindi / 1, 73 m), ndi odwala 7339 omwe akuchitika chifukwa cha odwala omwe adalandira mankhwala. Mankhwala ophunzirira (sitagliptin kapena placebo) adawonjezeredwa ku chithandizo chokhazikika malinga ndi momwe mayiko alili pano pakusankha mulingo wa HbA1C komanso kuwongolera ziwopsezo zamtima. Phunziroli lidaphatikizapo odwala 2004 omwe anali ndi zaka 75 ndi kupitirira (970 adatenga sitagliptin ndipo 1034 adatenga placebo). Zowopsa zonse zochitika zovuta za odwala omwe amatenga sitagliptin zinali zofanana ndi zomwe zimachitika kwa odwala omwe akuchita placebo. Kufufuza zovuta zomwe zadziwika kale ndi matenda ashuga kunavumbula zochitika zofananira pakati pa magulu, kuphatikizapo matenda (18,4% mwa odwala omwe amatenga sitagliptin ndi 17,7% mwa odwala omwe akuchitika). 1.4% mwa odwala omwe amatenga sitagliptin ndi 1.5% mwa odwala omwe akutenga placebo. Mbiri ya zochitika zovuta kwa odwala azaka zapakati pa 75 ndi zaka zambiri zinali zofanana ndi zomwe anthu ambiri amachita.

Mwa kuchuluka kwa odwala omwe adalandira chithandizo chamankhwala ("cholinga chochitira"), mwa iwo omwe adalandira chithandizo cha insulin ndi / kapena sulfonylureas, chiwopsezo cha hypoglycemia chinali 2.7% mwa odwala omwe amatenga sitagliptin, ndi 2, 5% mwa odwala omwe akumwa. Mwa odwala omwe sanalandire insulin ndi / kapena sulfonylurea, kuchuluka kwa hypoglycemia kunali 1.0% mwa odwala omwe amatenga sitagliptin ndi 0,7% mwa odwala omwe akutenga placebo. Zovuta zapansi zotsimikizika za kapamba anali 0.3% mwa odwala omwe amatenga sitagliptin ndi 0,2% mwa odwala omwe akutenga matenda. Zomwe zimachitika ndi khansa zomwe zimatsimikiziridwa kuti zimayambitsa khansa zinali 3.7% mwa odwala omwe amatenga sitagliptin ndi 4.0% mwa odwala omwe akutenga matenda.

Panthawi yolembetsanso kuyang'anira kugwiritsa ntchito sitagliptin mu monotherapy ndi / kapena kuphatikiza mankhwala ndi othandizira ena a hypoglycemic, zochitika zowonjezera zinadziwika. Popeza izi zidapezedwa mwakufuna kwa anthu opanda malire, ubale ndi zomwe zimachitika pakadali pano sizingadziwike. Izi zikuphatikiza:

Hypersensitivity reaction, kuphatikizapo anaphylaxis, angioedema, zidzolo, urticaria, khungu vasculitis, zotupa zakhungu, kuphatikizapo Stevens-Johnson syndrome, pachimake pancreatitis, kuphatikizapo hemorrhagic ndi necrotic mawonekedwe omwe amapha komanso osavulaza, kuwonongeka kwaimpso. kusakwanira (dialysis nthawi zina kumafunikira), matenda apumidwe am'mimba thirakiti, nasopharyngitis, kudzimbidwa, kusanza, kupweteka mutu, arthralgia, myalgia, kupweteka kwa miyendo, kupweteka kwa msana, kuyabwa, pemphigoid.

Zosintha mu ma laborator:

Kusinthasintha pafupipafupi kwa magawo a labotale m'magulu azithandizo a sitagliptin (mu tsiku ndi tsiku mlingo wa 100 mg) anali wofanana ndi pafupipafupi m'magulu a placebo. Kwambiri, koma osati mayesero onse azachipatala, panali kuwonjezeka pang'ono pa kuwerengera kwa leukocyte (pafupifupi 200 / comparedl poyerekeza ndi placebo, zomwe zili kumayambiriro kwa chithandizo chinali 6600 / μl) chifukwa cha kuchuluka kwa neutrophils.

Kusanthula kwa kachipangizidwe ka mankhwalawa kachipangizoka kanawonetsa kuwonjezeka pang'ono kwa kuchuluka kwa uric acid (pafupifupi 0,2 mg / dl poyerekeza ndi placebo), ambiri odzipereka asanalandire chithandizo anali 5-5,5 mg / dl) mwa odwala omwe amalandira sitagliptin pa mlingo wa 100 ndi 200 mg tsiku. Panalibe milandu yachitukuko cha gout. Kunali kuchepa pang'ono pa kuchuluka kwa zamchere kwambiri phosphatase (pafupifupi 5 IU / L poyerekeza ndi placebo, ndende yolimbitsa thupi isanakwane chithandizo anali 56-62 IU / L), pang'ono pokhudzana ndi kuchepa pang'ono kwa kachigawo kakang'ono ka mafupa a alkaline phosphatase.

Zosintha zomwe zidasungidwa mu magawo a labotale sizikuwoneka kuti ndizofunikira kwambiri.

Pophunzira pakukhudzana ndi mankhwala ena, sitagliptin sanakhale ndi vuto lililonse pama pharmacokinetics a mankhwala otsatirawa: metformin, rosiglitazone, glibenclamide, simvastatin, warfarin, kulera kwapakamwa. Kutengera ndi izi, sitagliptin sikuletsa CYP3A4, 2C8, kapena 2C9 isoenzymes. Kutengera ndi data ya in vitro, sitagliptin imalepheretsanso CYP2D6, 1A2, 2C19 ndi 2B6 isoenzymes ndipo simalimbikitsa CYP3A4 isoenzyme. Mobwerezabwereza makonzedwe a metformin osakanikirana ndi sitagliptin sizinakhudze kwambiri magawo a pharmacokinetic a sitagliptin mwa odwala omwe ali ndi matenda a shuga 2.

Malinga ndi kuchuluka kwa anthu omwe ali ndi pharmacokinetic kusanthula kwa odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga, chithandizo chothandizirana sichinawakhudze kwambiri pharmacokinetics ya sitagliptin. Kafukufukuyu adawunikira mitundu ingapo ya mankhwala omwe amagwiritsidwa ntchito kwambiri ndi odwala omwe ali ndi matenda a shuga 2, kuphatikizapo: lipid-kuchepetsa mankhwala (statins, fibrate, ezetimibe), antiplatelet agents (clopidogrel), antihypertensive mankhwala (ACE inhibitors, angiotensin II receptor antagonists, beta-blockers, blockers "pang'onopang'ono" calcium njira, hydrochlorothiazide), mankhwala osapweteka a antiidal (naproxen, diclofenac, celecoxib), antidepressants (bupropion, fluoxetine, sertraline), antihistamines (cetiri zine), proton pump inhibitors (omeprazole, lansoprazole) ndi mankhwala ochizira erectile dysfunction (sildenafil).

Panali kuwonjezeka pang'ono kwa AUC (11%), komanso Cmax (18%) ya digoxin akaphatikizidwa ndi sitagliptin. Kukula kumeneku sikumawerengedwa kuti ndikofunika m'thupi. Sitikulimbikitsidwa kuti musinthe mlingo wa digoxin kapena sitagliptin mutagwiritsidwa ntchito limodzi.

Kuwonjezeka kwa AUC ndi Cmax kwa sitagliptin kunadziwika ndi 29% ndi 68%, motero, mwa odwala omwe amaphatikiza mlingo umodzi wamkamwa wa 100 mg ya sitagliptin ndi mlingo umodzi wamkamwa wa 600 mg wa cyclosporin, potent inhibitor ya p-glycoprotein. Kusintha koonekera mu pharmacokinetic machitidwe a sitagliptin sikuwoneka ngati ofunikira. Kusintha kwa mlingo wa Xelevia sikulimbikitsidwa mutaphatikizidwa ndi cyclosporine ndi zina za p-glycoprotein inhibitors (mwachitsanzo ketoconazole).

Kafukufuku wopanga kuchuluka kwa anthu odwala komanso odzipereka athanzi (N = 858) pamankhwala osiyanasiyana (N = 83, pafupifupi theka lake lomwe limafotokozedwa ndi impso) sanawonetse zazomwe zimachitika chifukwa cha mankhwala a pharmgokinetics a sitagliptin.

Mlingo wa Xelevia

Mlingo wovomerezeka wa Xelevia ndi 100 mg kamodzi pakamwa monga monotherapy, kapena kuphatikiza ndi metformin, kapena zotumphukira za sulfonylurea, kapena PPAR-γ agonists (thiazolidinediones), kapena insulin (wokhala ndi kapena wopandaformform), kapena kuphatikiza ndi metformin ndi zotumphukira za sulfonylurea, kapena metformin ndi agonists a PPAR-γ.

Xelevia imatha kuthandizidwa popanda kudya. Mlingo wa metformin, zotumphukira za sulfonylurea ndi PPAR-γ agonists ziyenera kusankhidwa kutengera mtundu waukulu wa mankhwalawa.

Mukaphatikiza Xelevia ndi zotumphukira za sulfonylurea kapena insulin, ndikofunikira kuti muchepetse mankhwala omwe amapezeka kuti ndi a sulfonylurea kapena a insulin omwe angapangitse kuti achulukane ndi hypoglycemia wa sulfony.

Wodwala akaphonya kumwa mankhwala a Xelevia, mankhwalawo amayenera kumwedwa msanga wodwala akakumbukira mankhwala omwe adasowa.

Sizovomerezeka kumwa kawiri mlingo wa Xelevia tsiku lomwelo.

Odwala aimpso kulephera:

Odwala omwe ali ndi vuto lochepa la impso (creatinine chilolezo (CC) & gt50 ml / mphindi, pafupifupi lofanana ndi kuchuluka kwa serum creatinine ndende ya & lt1.7 mg / dl mwa amuna ndi & lt1.5 mg / dl mwa akazi) safuna kusintha kwa mlingo wa Xelevia.

Chifukwa chakufunika kusintha kwa mtundu wa sitagliptin mwa odwala omwe ali ndi kuchepa kwambiri kwa aimpso, kugwiritsa ntchito Xelevia sikumawonetsedwa m'gulu ili la odwala (kusowa kwa zoopsa piritsi la 100 mg ndi kusowa kwa 25 mg ndi 50 mg Mlingo salola mlingo wake wa odwala omwe ali ndi impso. kusakwanira kwakanthawi komanso koopsa).

Chifukwa cha kufunika kosintha kwa mlingo, tikulimbikitsidwa kuti odwala omwe ali ndi vuto la impso ayambe kuwunika ntchito ya impso asanayambe chithandizo ndi sitagliptin komanso nthawi yamankhwala.

Odwala omwe ali ndi vuto la chiwindi:

Palibe kusintha kwa mlingo wa Xelevia kwa odwala ofatsa kuti azichita pang'ono kwa chiwindi. Mankhwala sanaphunziridwe kwa odwala omwe ali ndi vuto lalikulu la chiwindi.

Palibe kusintha kwa mlingo kwa Xelevia komwe kumafunikira odwala okalamba.

Panthawi ya mayesero azachipatala podzipereka, thanzi limodzi la 800 mg la sitagliptin nthawi zambiri limalekerera. Kusintha kocheperako pakatikati pa QTc, kosawoneka ngati kofunika kwambiri, kunawonedwa mu maphunziro amodzi a sitagliptin pa mlingo wa 800 mg patsiku. Mlingo woposa 800 mg patsiku kwa anthu sunaphunzire.

Mu gawo loyamba la mayesero azachipatala, Mlingo wambiri wazovuta zilizonse zomwe zimagwirizana ndi chithandizo cha mankhwala ndi sitagliptin sizinachitike pakumwa mankhwala tsiku lililonse mpaka 400 mg kwa masiku 28.

Pankhani ya mankhwala osokoneza bongo, ndikofunikira kuyambitsa njira zothandizira: kuchotsa mankhwalawa osagwiritsidwa ntchito m'mimba, kuwunika mayendedwe ofunikira, kuphatikiza ECG, komanso kukhazikitsidwa kwa mankhwala othandizira, ngati pakufunika kutero.

Sitagliptin salemala bwino. M'maphunziro azachipatala, ndi 13.5% yokha ya mankhwala omwe amachotsedwa m'thupi panthawi ya dialysis ya maola atatu. Kutalika kwa dialysis kumatha kutumikiridwa ngati pakufunika. Palibe umboni wotsimikiza za kugwira ntchito kwa peritoneal dialysis kwa sitagliptin.

Njira yayikulu yodziwirira ya sitagliptin kuchokera ku thupi ndi impso. Kuti akwaniritse plasma wozungulira monga odwala omwe ali ndi vuto la impso, odwala omwe ali ndi impso kwambiri, komanso odwala omwe ali ndi vuto loti aimpso ofunika a hemodialysis kapena peritoneal dialysis, kusintha kwa Xelevia kumafunikira .

Pakhala lipoti lachitukuko cha pancreatitis pachimake, kuphatikizapo hemorrhagic kapena necrotic yotsitsa komanso yopanda vuto, mwa odwala omwe amatenga sitagliptin. Odwala ayenera kudziwitsidwa za mawonekedwe a pancreatitis yapakati: kulimbikira, kupweteka kwambiri pamimba. Mawonetseredwe azachipatala a kapamba anazimiririka atasiya ntchito ya sitagliptin. Pankhani ya pancreatitis yomwe ikukayikira, ndikofunikira kusiya kumwa Xelevia ndi mankhwala ena oopsa.

Malinga ndi mayesero azachipatala a sitagliptin, kuchuluka kwa hypoglycemia nthawi ya monotherapy kapena kuphatikiza mankhwala omwe samayambitsa hypoglycemia (metformin, pioglitazone) anali ofanana ndi zochitika za hypoglycemia pagulu la placebo. Monga mankhwala ena a hypoglycemic, hypoglycemia imawonedwa ndi sitagliptin limodzi ndi insulin kapena zotumphukira za sulfonylurea. Pofuna kuchepetsa mwayi wokhala ndi hypoglycemia wa sulfone, mlingo wa zotumphukira za sulfonylurea ziyenera kuchepetsedwa.

Gwiritsani ntchito mwa okalamba:

M'maphunziro azachipatala, kufunikira ndi chitetezo cha sitagliptin mwa odwala okalamba (? Zaka 65, odwala 409) anali ofanana ndi omwe ali ndi odwala ochepera zaka 65. Kusintha kwa Mlingo malinga ndi zaka sikofunikira. Odwala okalamba amatha kukhala ndi kulephera kwa impso. Chifukwa chake, monga m'mibadwo ina yonse, kusintha kwa mankhwalawa ndikofunikira kwa odwala omwe ali ndi vuto laimpso.

Sitagliptin Cardiovascular Safety Assessment Study (TECOS):

Kutulutsa mawonekedwe, kapangidwe kake ndi ma CD

Zimapangidwa mwanjira ya beige, mapiritsi a biconvex mu zokutira filimu. Zopangidwa:

sitagliptin phosphate monohydrate (100 mg sitagliptin),
calcium hydrogen phosphate osakhudzidwa,
cellcrystalline mapadi,
sodium stearyl fumarate
sodium croscarmellose,
magnesium wakuba.

Mapiritsi 14 ali ndi chotupa (2 mu katoni).

Kuyanjana kwa mankhwala osokoneza bongo

Palibe chofunikira pakuwonetsetsa kwa othandizira ena pa Xelevia adapezeka. Chifukwa chake, izi sizifunikira kusintha kwa iwo. Kupatula kwake ndi sulfonylurea ndi insulin.

Sitagliptin siyimakhudza kugwira ntchito kwa mankhwala owonjezera. Panalibe kuyanjana kwakukulu pakuphatikizira mankhwala ndi othandizira ena.

Komabe, pofuna kupewa ngozi, popereka mankhwala, katswiri ayenera kudziwitsidwa za mankhwalawa.

Malangizo apadera

Pofuna kupewa hypoglycemia, tikulimbikitsidwa kuchepetsa mlingo wotengedwa ndi mankhwala ena a hypoglycemic.

Ndikofunikira kuti anthu okalamba azaka zopitilira 65 aziona momwe impso zikuyendera, popeza chiwalochi chimakonda kuthana ndi zovuta. Odwala oterewa amatha kukhala ndi hypoglycemia panthawi yofanana ndi mankhwala ena ofanana.

Palibe zotsatira pa mtima.

Chomwe chimagwira chokha sichikhudza kuwongolera makina kapena kugwira ntchito ndi makina. Komabe, kuphatikiza mankhwala, izi zimachitika. Chifukwa chake, pankhaniyi, ndibwino kusiya kuyendetsa.

Imatulutsidwa kokha pamankhwala!

Fananizani ndi fanizo

Januvius. Mankhwala ozikidwa ku sitagliptin. Amapanga kampani "Merck Sharp", Netherlands. Mtengo wa ma CD udzakhala ma ruble 1600 ndikukwera. Chochita choperekedwa ndi chida ichi ndi chofanana ndi Xelevia. Ndi machitidwe a incretin mimetic, omwe amakhudza shuga wamagazi ndikuchepetsa chilimbikitso cha munthu wodwala matenda ashuga. Chifukwa chake, nthawi zambiri amalembera anthu omwe ali ndi kunenepa kwambiri ngati matenda am'mbali. Mwa mphindi - mtengo. Uwu ndi mndandanda wathunthu.

Yasitara. Mapiritsi okhala ndi sitagliptin mu kapangidwe kake. Wopanga ndi Pharmasintez, Russia. Mofanizira analogue wa mankhwala, omwe ali ndi vuto lofanananso ndi zotsutsana.Mtengo wokwanira wa gulu ili. Ndiosavuta kupangira chithandizo, popeza ili ndi mitundu itatu ya mankhwala - 25, 50 ndi 100 mg ya sitagliptin. Komabe zoletsedwa kwa amayi apakati ndi ana. Pakati pa mphindi - nthawi zambiri zimayambitsa hypoglycemia.

Vipidia. Komanso ndi machitidwe a incretin, koma ali ndi apogliptin. Amapezeka mu mapiritsi a 12,5 ndi 25 mg. Mtengo - kuchokera ku 800 mpaka 1150 ma ruble, kutengera mlingo. Yopangidwa ndi Takeda GmbH, Japan. Zochita zake ndizofanana, koma zothandiza kwambiri. Osamalembera ana ndi amayi apakati chifukwa chosowa kafukufuku. Ma contraindication odziwika komanso mndandanda wazotsatira zoyipa.

Attokana. Mategliflozin mapiritsi. Amapanga kampani yaku Italiya Janssen-Silag. Mtengo wake ndiwokwera: kuchokera ku ruble 2600 pachidutswa cha 100. Amagwiritsidwa ntchito pochiza matenda a shuga ndi kusakwanira kwa metformin komanso zakudya. Komabe, chithandizo chamankhwala chiyenera kuphatikizidwa ndi chakudya chosankhidwa ndi adokotala. Contraindication ndi muyezo.

Galvus Met. Uku ndi kuphatikiza kwa matenda ashuga, pomwe zotsatira za chinthu chimodzi sizikwanira. Wopangidwa ndi metformin ndi vildagliptin. Mapiritsi amapangidwa ndi kampani yaku Swiss Novartis. Mtengo - kuchokera ku ma ruble 1500 ndi pamwamba. Zotsatira zake ndizitali, pafupifupi maola 24. Sizingagwiritsidwe ntchito pochiza ana, amayi oyembekezera komanso oyembekezera. Mu okalamba, imagwiritsidwa ntchito mosamala. Sikoyenera monga m'malo mwa insulin.

Trazenta. Mankhwalawa ali ndi linagliptin, amenenso ndi choletsa DPP-4. Chifukwa chake, machitidwe ake ali ofanana ndi Xelevia. Ndibwino kuti mumapezeka m'matumbo, ndiye kuti, kupsinjika kochepa kumapangidwa pa impso. Itha kugwiritsidwa ntchito limodzi ndi mankhwala ena. Zoletsa kuvomereza ndizofanana. Palinso zovuta zambiri. Mtengo - kuchokera ku 1500 rubles. Amapanga kampani "Beringer Ingelheim Pharma" ku Germany ndi USA.

Kusinthira ku mankhwala ena kumachitika kokha ndi dokotala. Kudzichitira nokha mankhwala ndikosavomerezeka!

Mwambiri, anthu odwala matenda ashuga amalankhula motsimikiza za mankhwalawa. Kuchita kwake kwambiri komanso kupezekako mosavuta kumadziwika. Kwa ena, mankhwalawa sanali oyenera.

Valery: “Poyamba ndinkagwiritsa ntchito Galvus, ndimaikonda kwambiri. Koma kenako adasiya kumupatsa mwayi kuchipatala kuti andipindule, ndipo adotolo adandilangiza kuti ndisinthe ku Xelevia. Sindinazindikire kusiyana. Amagwira ntchito mofananamo, monga adokotala anafotokozera. Shuga ndi wabwinobwino, sindimayang'anira kudumphadumpha. Munthawi yamankhwala, "zoyipa" sizinachitike. Ndimakondwera ndi mankhwalawa. ”

Alla: “Dokotalayo adawonjezeranso Xelevia ndi insulini, chifukwa zakale sizinali kulimbana ndi shuga nthawi zonse. Kota itachepetsa mlingo wake, ndidayamba kumva bwino kwambiri. Zizindikiro sizikudumpha, mayesowa ndiabwino, komanso mkhalidwe wazachipatala. Ndinaonanso kuti ndikufuna kudya zochepa. Dokotalayo adalongosola kuti mankhwalawa onse amtundu wamtunduwu amachita mwanjira iyi. Ndiye chimenecho ndi chowonjezera. "